EP 3351551 A4 20190515 - PREPARATION METHOD OF NUCLEOSIDE PHOSPHORAMIDATE PRODRUGS AND INTERMEDIATES THEREOF
Title (en)
PREPARATION METHOD OF NUCLEOSIDE PHOSPHORAMIDATE PRODRUGS AND INTERMEDIATES THEREOF
Title (de)
VERFAHREN ZUR HERSTELLUNG VON NUKLEOSID-PHOSPHORAMIDAT-PRODRUGS UND ZWISCHENPRODUKTE DAVON
Title (fr)
PROCÉDÉ DE PRÉPARATION DE PROMÉDICAMENTS DE PHOSPHORAMIDATE DE NUCLÉOSIDE ET PRODUITS INTERMÉDIAIRES CORRESPONDANTS
Publication
Application
Priority
- CN 201510588122 A 20150916
- CN 2016098846 W 20160913
Abstract (en)
[origin: EP3351551A1] Provided in the present disclosure are a novel preparation method of nucleoside phosphoramidate prodrugs and the intermediates thereof. In particular, the method is adopted to perform isomer separation on the reaction product from a first step and then perform a two-step chemical synthesis, so as to prepare a high-purity compound S p -1. The method has simple and convenient operation and low cost. The prepared resulting single isomer S p -1 has high purity, and the HPLC purity thereof is 95% or more, and further, 99% or more. The method is suitable for industrial production and can satisfy the need of clinical study. Further, also provided in the present disclosure are a key intermediate phosphorus reagent for preparing the high-purity compound S p -1 and the preparation method thereof.
IPC 8 full level
C07H 19/10 (2006.01); C07F 9/24 (2006.01); C07H 1/00 (2006.01); C07H 1/02 (2006.01)
CPC (source: EP KR US)
A61P 35/00 (2017.12 - EP); C07F 9/24 (2013.01 - EP KR US); C07H 1/00 (2013.01 - KR US); C07H 1/02 (2013.01 - EP US); C07H 19/10 (2013.01 - EP KR US); Y02P 20/55 (2015.11 - EP)
Citation (search report)
- [Y] WO 2012075140 A1 20120607 - PHARMASSET INC [US], et al
- [Y] WO 2013187978 A1 20131219 - NANJING MOLECULAR RES INC [CN], et al
- [Y] US 2013288997 A1 20131031 - ROSS BRUCE S [US], et al
- [Y] MAGDALENA SLUSARCZYK ET AL: "Application of ProTide Technology to Gemcitabine: A Successful Approach to Overcome the Key Cancer Resistance Mechanisms Leads to a New Agent (NUC-1031) in Clinical Development", JOURNAL OF MEDICINAL CHEMISTRY, vol. 57, no. 4, 14 February 2014 (2014-02-14), US, pages 1531 - 1542, XP055568914, ISSN: 0022-2623, DOI: 10.1021/jm401853a
- See references of WO 2017045582A1
Designated contracting state (EPC)
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
DOCDB simple family (publication)
EP 3351551 A1 20180725; EP 3351551 A4 20190515; EP 3351551 B1 20221207; AU 2016322374 A1 20180322; AU 2016322374 B2 20200702; CA 2997203 A1 20170323; CA 2997203 C 20220531; CN 106543252 A 20170329; JP 2018528957 A 20181004; JP 6731477 B2 20200729; KR 102226164 B1 20210310; KR 20180053320 A 20180521; US 2018237466 A1 20180823; WO 2017045582 A1 20170323
DOCDB simple family (application)
EP 16845696 A 20160913; AU 2016322374 A 20160913; CA 2997203 A 20160913; CN 201510588122 A 20150916; CN 2016098846 W 20160913; JP 2018512893 A 20160913; KR 20187008621 A 20160913; US 201615753734 A 20160913